Tesamorelin là một chất tương tự hormone phát hành hormone tăng trưởng (GHRH) bao gồm GHRH tiêu chuẩn mà một nhóm axit trans-3anoic bổ sung đã được thêm vào. Được sản xuất bởi Theratechnologies của Canada, Tesamorelin đã trở thành loại thuốc mới nhất được FDA phê duyệt để sử dụng trong bệnh nhân tim liên quan đến HIV vào năm 2010.

Trình tự (chữ cái đơn):Unk-ala-asp-ala-eight-thhr-asn-ser-try-arg-light-val-lie-gln-gln-gln-ln-leu-ser-ela-arg-light-light Eu-leu-gln-asp-iie-met-ser-arg-gln-gln-glu-glu-ser-asn-glu-glu-arg-glu-glu-ala-arg-ala-arg-leu
Công thức phân tử:C₂₂₃H₃₇₀N₇₂O₆₉S
Trọng lượng phân tử:5195.908 g/mol
PubChem CID: 44147413
Số CAS:901758-09-6

Như mộtTội lỗiTương tự, Tesamorelin có tất cả các tác dụng giống như các chất tương tự GHRH và GHRH nhưSermorelin, GRF (1-29), CJC-1295, v.v ... Việc bổ sung axit trans-3-hexanoic vào tesamorelin làm cho nó ổn định hơn trong huyết tương của con người và do đó làm tăng thời gian bán hủy của nó. Mặc dù sự gia tăng trong thời gian bán hủy, Tesamorelin, như CJC-1295, bảo tồn tác dụng sinh lý của GHRH và do đó có ít tác dụng phụ hơn so với các phân tử tương tự xóa bỏ hormone tăng trưởng xung (GH) bình thường.

Tesamorelin và Lypodystrophy

Việc sử dụng chính cho Tesamorelin là trong điều trị bệnh tim cô ấy liên quan đến HIV, phát sinh cả do nhiễm HIV và là tác dụng phụ của liệu pháp kháng retrovirus. Trong chứng ngủ mỡ, chất béo tích tụ quá mức cả trong bụng và ở các khu vực khác của cơ thể. Cơ chế sinh lý chịu trách nhiệm cho điều này không được hiểu rõ ràng, nhưng người ta cho rằng các chất ức chế protease thường được sử dụng^[1].

Patients suffering from lipodystrophy initially had diet, exercise, and a handful of ineffective medications to rely on for treatment. If those did not work, surgery was a last-ditch, often ineffective, and frequently complicated solution. In 2010, however, the FDA approved tesamorelin specifically for the treatment of HIV-associated lipodystrophy. The drug has been found to reduce adiposity by nearly 20% in this population [1]. Research suggests that tesamorelin is approximately 4 times more effective in reducing adiposity than all of the other available therapies combined ^[2].

Tesamorelin Investigated in Cardiac Disease

People with HIV are at increased risk of developing cardiovascular disease (CVD), in part due to abnormal fat deposition and in part due to the actions of antiretroviral drugs themselves. Prevention of CVD in HIV-positive individuals is considered to be the most important medical intervention for long-term well-being, after highly active antiretroviral therapy (HAART) of course. Until recently, statins have been the cornerstone of medical management in this population.

Research shows that tesamorelin, in addition to decreasing lipodystrophy, also reduces triglyceride levels, total cholesterol levels, and non-HDL-C levels in HIV-positive patients. A 15% reduction in visceral adipose tissue by tesamorelin correlates with a 50 mg decrease in trigylceride levels^{[3], [4]}.

Changes in triglyceride levels of HIV-positive patients who respond to tesamorelin.
Source: PubMed

It is worth noting that ectopic fat deposition, as seen in lipodystrophy, is associated with inflammation. Inflammation of any kind is a risk factor for CVD. Visceral adipose tissue, liver fat, and epicardial fat are all independently associated with increased risk of CVD. By reducing ectopic fat deposition, tesamorelin directly decreases inflammation and an individual’s risk for CVD.

Growth Hormone Deficiency and HIV

Recent evidence suggests that HAART is associated with a number of endocrine and metabolic problems, including growth hormone (GH) deficiency. It appears that the pituitary gland is altered in HIV infection and, as a consequence, approximately one third of patients with HIV who are taking HAART have GH deficiency^[5]. This may, to some extent, explain why lipodystrophy is so common in individuals with HIV and also why tesamorelin is such an effective treatment. Tesamorelin is a safer and more effective way to raise GH levels than administration of exogenous GH, particularly in HIV-positive individuals.

Tesamorelin for Peripheral Nerve Damage

Peripheral nerve damage can be a consequence of injury, diabetes, or even surgical interventions. It often results in debilitating problems with both motor and sensory function in the affected area, but there is little that can be done to correct the problem because nerve cells are notoriously difficult to regenerate. Research, however, suggests that therapies based on growth hormone manipulation may improve peripheral nerve injury and increase both rate and extent of healing^[6]. Tesamorelin is currently the leading candidate for such intervention, in part because it already has FDA approval.

Tesamorelin Investigated in Dementia

There is now evidence to suggest that GHRH analogues, like tesamorelin, are effective in enhancing cognition in patients suffering from the early stages of dementia. A large, randomized, double-blind, placebo-controlled study at the University of Washington School of Medicine, carried out over twenty weeks, suggests that tesamorelin and other GHRH analogues may impact dementia by increase gamma-aminobutyric acid (GABA) levels in the brain and by decreasing myo-insoitol (MI) levels^[7]. These findings open up a pathway for using tesamorelin in the treatment of dementia, but also suggest new areas for scientists to explore as they look for a cure or a preventative.

Tesamorelin improves both executive function and verbal memory in patients suffering from mild cognitive impairment.
Source: PubMed

Because it is FDA approved for use in humans, tesamorelin is an attractive peptide for ongoing clinical research. It is currently under review for its ability to reduce cardiovascular disease in HIV, improve healing of peripheral nerves following injury, and slow the progression of dementia. Clinical trials are already underway in several different areas.

Tesamorelin exhibits minimal side effects, low oral and excellent subcutaneous bioavailability in mice. Per kg dosage in mice does not scale to humans. Tesamorelin for sale at

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

1. Clinical Review Report: Tesamorelin (Egrifta). Ottawa (ON): Canadian Agency for Drugs and Technologies in Health, 2016.
2. A. Mangili, J. Falutz, J.-C. Mamputu, M. Stepanians, and B. Hayward, “Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat,” PloS One, vol. 10, no. 10, p. e0140358, 2015. [PubMed]
3. J. Falutz et al., “Metabolic effects of a growth hormone-releasing factor in patients with HIV,” N. Engl. J. Med., vol. 357, no. 23, pp. 2359–2370, Dec. 2007. [NEJM]
4. T. L. Stanley et al., “Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving tesamorelin,” Clin. Infect. Dis. Off. Publ. Infect. Dis. Soc. Am., vol. 54, no. 11, pp. 1642–1651, Jun. 2012. [PubMed]
5. V. Rochira and G. Guaraldi, “Growth hormone deficiency and human immunodeficiency virus,” Best Pract. Res. Clin. Endocrinol. Metab., vol. 31, no. 1, pp. 91–111, 2017. [PubMed]
6. S. H. Tuffaha et al., “Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury,” Expert Opin. Ther. Targets, vol. 20, no. 10, pp. 1259–1265, Oct. 2016. [PubMed]
7. S. D. Friedman et al., “Growth hormone-releasing hormone effects on brain γ-aminobutyric acid levels in mild cognitive impairment and healthy aging,” JAMA Neurol., vol. 70, no. 7, pp. 883–890, Jul. 2013. [PubMed]

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